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Agomelatine transdermal patch as well as preparation method and application thereof

A transdermal patch and patch technology, applied in the field of medicine, can solve problems such as low bioavailability, and achieve the effects of high bioavailability, good stability and improved solubility

Pending Publication Date: 2022-02-15
江苏山信药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Oral preparations of agomelatine are mainly metabolized by the liver, have obvious hepatic first-pass effect, have very low bioavailability (absolute bioavailability <5%), and have obvious side effects

Method used

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  • Agomelatine transdermal patch as well as preparation method and application thereof
  • Agomelatine transdermal patch as well as preparation method and application thereof
  • Agomelatine transdermal patch as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] The preparation of embodiment 1 agomelatine transdermal patch

[0076] Composition of agomelatine transdermal patch:

[0077]

[0078] The preparation method of agomelatine transdermal patch comprises the following steps:

[0079] 1) Weigh the required amount of agomelatine and add it to ethanol, stir at 25°C and 200rpm for 20min, then add octyl salicylate, N-methylpyrrolidone, vitamin E, polyacrylate-13, 25°C , Stirring at 200rpm for 20min to obtain a mixture;

[0080] 2) Spread the mixture on non-woven fabric or tape, cut into 2.2cm 2 (containing 2 mg agomelatine), put it in a drying oven, cure at 60°C for 30 minutes, take it out and apply an anti-adhesive layer, seal it, and get it.

Embodiment 2

[0081] The preparation of embodiment 2 agomelatine transdermal patch

[0082] Composition of agomelatine transdermal patch:

[0083]

[0084] The preparation method of agomelatine transdermal patch comprises the following steps:

[0085] 1) Weigh the required amount of agomelatine and add it to ethanol, stir at 25°C and 200rpm for 20min, then add dimethyl sulfoxide, dimethylacetamide, xanthan gum, BHT in turn, at 25°C and 200rpm Stir for 20min to obtain a mixture;

[0086] 2) Spread the mixture on non-woven fabric or tape, and cut into 2.2cm 2 (containing 4 mg agomelatine), put it in a drying oven, solidify at 80°C for 30 minutes, take it out and apply an anti-adhesive layer, seal it, and get it.

Embodiment 3

[0087] The preparation of embodiment 3 agomelatine transdermal patch

[0088] Composition of agomelatine transdermal patch:

[0089]

[0090] The preparation method of agomelatine transdermal patch comprises the following steps:

[0091] 1) Weigh the required amount of agomelatine and add it to ethyl acetate, stir at 25°C and 200rpm for 20min, then add octyl salicylate, liquid paraffin, simethicone, BHT, polyisobutylene in sequence, at 25°C, Stir at 200rpm for 20min to obtain a mixture;

[0092] 2) Spread the mixture on non-woven fabric or tape, and cut into 2.2cm 2 (containing 4 mg agomelatine), put it in a drying oven, cure at 70°C for 10 minutes, take it out and apply an anti-adhesive layer, seal it, and get it.

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Abstract

The invention relates to an agomelatine transdermal patch and a preparation method thereof. The agomelatine transdermal patch comprises 1-10% (w / w) of agomelatine or pharmaceutically acceptable salt thereof, 1-20% (w / w) of a penetration enhancer, 1-15% (w / w) of a colloid softener or humectant or crystal inhibitor, 30-70% (w / w) of a polymer matrix and 10-50% (w / w) of a solvent. According to the agomelatine transdermal patch, the components and the proportion of the agomelatine transdermal patch are scientifically screened, the solubility of agomelatine is remarkably improved, the agomelatine transdermal patch has the advantages of being good in stability, high in uniformity, high in bioavailability, good in patient compliance, free of skin irritation and the like, and the effectiveness and the safety of drugs are remarkably improved.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an agomelatine transdermal patch, a preparation method and an application thereof. Background technique [0002] Agomelatine (Agomelatine, N-[2-(7-methoxynaphthalene-1-yl)ethyl]acetamide, C 15 h 17 NO 2 ) is an antidepressant, which mainly treats adult depression clinically. [0003] [0004] The oral preparation of agomelatine is mainly metabolized by the liver, has obvious hepatic first-pass effect, has very low bioavailability (absolute bioavailability <5%), and has obvious side effects. After taking agomelatine tablets, some patients experienced side effects such as nausea, dizziness, blurred vision, abdominal pain, bloating, diarrhea, and constipation, and even caused liver function damage, elevated transaminases, and jaundice. There is an urgent need for new dosage forms with higher bioavailability and fewer side effects in clinical practice. Contents of the invention ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K31/165A61P25/24
CPCA61K31/165A61K9/703A61P25/24
Inventor 林山朱明哲孔德义
Owner 江苏山信药业有限公司
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